a neuronal nicotinic AChR antagonist. Potent ganglioblocker. Hypotensive. Good penetration of biological membranes. Rigid bicyclic analog of Pempidine. Non-quaternary analog of Quirestine.

Quinicludine derivative, C₁₁H₂₁N .HBr, synthetic.

• Molecular Weight : 248.20 Da.
  
  
• Melting Point : 269-273 °C.
  
  
• Solubility in : water, ethanol (1 g in 10 ml).
  
  
• Purity min. : min. 99.5%.
  TLC (Silufol UV-254, MeOH:NH3(25%) Rf 0.1, development with Dragendorff¨ reagent); NMR (D2O).
  
  
• Physical Form : colorless crystal powder.
  
  
• Chemical Name : 2,2,6,6-tetramethylquinicludine hydrobromide.
  
  
• Biological Activity : For comparative information see the attached 2 tables.
  Cell permeant central nicotinic acetylcholine receptor blocker without action on skeleton muscle innervation. Quinuclidine analog of Pempidine, non-quaternary analog of Quirestine. Hypotensive, selectively blocks autonomic ganglia, the adrenal medulla, carotid glomerules.
  
  Three-fold more active than Pempidine, wide therapeutic range [1]. Slows down neuronal pre- and post ganglionar transmission: dilates peripheral vessels and bronchi, arterial pressure and pressor reaction drop. Suppresses gland secretion. Sedative.
  
  Good penetration of biological membranes.
  
  Blocks superior cervical sympathetic ganglion (electrical stimulation of cats nictiating membrane): ED₅₀ = 17 µg/kg , Pempidine 54 µg/kg.
  
  Blocks autonomic ganglion ( vagus electrical stimulation): depressor reaction suppression - 50 µg /kg 40%, 500 µg/kg 100%. After 100% nicotinic blockade with 500 µg /kg, cardiac system still reacts to muscarinic action of ACh (i.v.).
  
  
• Toxicity (LD₅₀) : mice (orally): 345 mg/kg.
  
  
• Storage recommendations : store at room temperature. Solution for use: dissolve in water: 10-³M (2 mg in 8.06 ml), stable for 1-2 days at 20°C.
  
  
• Safety recommendations : do not swallow or inhale; avoid eye and skin contact.
  
  
• CAS Reg. No. : 30015-57-7
  
  
• Bibliography :
  
  1. Mashkovsky M.D. et al., "Further developments in research on the chemistry and pharmacology of synthetic quinuclidine derivatives." Progr. Drug. Res., (1983). 27:9-61
  2. Sharapov I.V., Farm, Toksikol. (1972). (Russian). (6):687-690
  3. Nikitskaya E.S. et al., Khim. Farm. Zh. (1970) (Russian) (10):58-61
  4. Shubina L.A., Sovetskaya Med. (1968) (Russian). (10):87-92
  5. Nogaller A.M. et al., Klinitcheskaya Med. (1975) (Russian). (10):52-56